EP 4223762 A1 20230809 - METHOD FOR PRODUCING 4-BORONO-L-PHENYLALANINE AND INTERMEDIATE THEREOF
Title (en)
METHOD FOR PRODUCING 4-BORONO-L-PHENYLALANINE AND INTERMEDIATE THEREOF
Title (de)
VERFAHREN ZUR HERSTELLUNG VON 4-BORONO-L-PHENYLALANIN UND ZWISCHENPRODUKT DAVON
Title (fr)
PROCÉDÉ DE PRODUCTION DE 4-BORONO-L-PHÉNYLALANINE ET D'UN INTERMÉDIAIRE DE CELUI-CI
Publication
Application
Priority
- JP 2020189349 A 20201113
- JP 2021040947 W 20211108
Abstract (en)
A method for producing 4-borono-L-phenylalanine and its intermediates is provided.The method is for producing a compound represented by formula (II) from a compound represented by formula (I),wherein, in formulas (I) and (II),X represents Cl, F, Br, or I, R<sup>1</sup> represents NR<sup>11</sup>R<sup>12</sup>, R<sup>11</sup> represents H or a protective group of an amino group, R<sup>12</sup> represents a protective group of an amino group, R<sup>2</sup> represents COOR<sup>21</sup>, R<sup>21</sup> represents H or a linear or branched C1 to C10 alkyl group or benzyl group, R<sup>3</sup> represents H or COOR<sup>31</sup>, and R<sup>31</sup> represents a linear or branched C1-C10 alkyl group or a benzyl group; R<sup>4</sup> represents either boronic acid (B(OH)<sub>2</sub>), boronic acid ester or boronic acid amide;Provided is a method of production comprising: a first step in which a compound represented by formula (I) reacts with a linear or branched C1-C10 alkylmagnesium halide in the presence of a metal halide; and a second step in which a boronic acid ester or boronic acid amide reacts with the compound obtained in said first step.
IPC 8 full level
C07F 5/02 (2006.01)
CPC (source: EP KR US)
C07F 5/025 (2013.01 - EP KR US); Y02P 20/55 (2015.11 - EP KR)
Citation (search report)
See references of WO 2022102565A1
Designated contracting state (EPC)
AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
Designated extension state (EPC)
BA ME
Designated validation state (EPC)
KH MA MD TN
DOCDB simple family (publication)
EP 4223762 A1 20230809; AU 2021377857 A1 20230622; CN 116113636 A 20230512; JP WO2022102565 A1 20220519; KR 20230107791 A 20230718; TW 202229229 A 20220801; US 2023416280 A1 20231228; WO 2022102565 A1 20220519
DOCDB simple family (application)
EP 21891811 A 20211108; AU 2021377857 A 20211108; CN 202180062978 A 20211108; JP 2021040947 W 20211108; JP 2022561897 A 20211108; KR 20237009241 A 20211108; TW 110142148 A 20211112; US 202118252305 A 20211108